US 2011/0086799 A1 · GnRH II Analogs and Uses Thereof in the Immune System

Abstract

Specially designed GnRH II analogs that are resistant to degradation by peptidases, are disclosed. The GnRH II analogs incorporate D-Arg, D-Leu, D-tBu-Ser, D-Trp, D-Asn or other active D amino acids at position 6 and aza-Gly-amide or other amino acid-amide at position 10. The D-Arg (6)—GnRH II-aza-Gly (10)-amide, D-Asn—GnRH II-aza-Gly (10)-amide, and D-Leu(6)—GnRH II-aza-Gly(10)-amide analogs are also provided, and demonstrate preferential binding to immune system GnRH receptors. These GnRH II analogs or their antibodies may be used in pharmaceutical preparations, and specifically in treatment of various immune system disorders. Antibodies to GnRH II, Applicant's GnRH TI analogs, and GnRH receptors can be used for the detection of GnRH II or the GnRH II analog or the GnRH II receptors as a diagnostic tool and/or to monitor treatment.

Claims30

Dependent claims

A gonadotropin releasing hormone II analog having the sequence as defined in SEQ ID NO:

3, p-Glu-His-Trp-Ser-His-Xaa-Trp-Tyr-Pro-Xaa, said analog comprising a D-amino acid substitution at position 6 and an aza-Gly-amide substitution, or other amino acid-amide substitution at position 10;
wherein said analog resists degradation by post-proline peptidases and endopeptidases in immune tissues and other tissues where immune cells or immune tissues are found;
wherein said analog binds with higher affinity to gonadotropin releasing hormone receptors in the immune system than native gonadotropin releasing hormone I or native gonadotropin releasing hormone II;
and
wherein said analog is a non-chimaeric analog of gonadotropin releasing hormone II.

2 more elements

Dependencies are inferred from the claim text.

GnRH II Analogs and Uses Thereof in the Immune System

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GnRH II Analogs and Uses Thereof in the Immune System

Life of this patent

Abstract

Claims30